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Opioid
Mod 4
Question | Answer |
---|---|
MORPHINE | Full Agonist |
MEPERIDINE | Full Agonist |
METHADONE | Full Agonist treat addicts euphoria not as great |
PENTAZOCINE | Mixed Agonist-antagonist kappa, delta abuse potential Talwin = aspirin Talacen = acetminophen |
BUPRENORPHINE | Mixed Agonist-antagonist high Mu |
OXYCODONE | Partial Agonist |
CODEINE | Partial Agonist Tylenol 2,3,4 - w/ acetaminophen |
HYDROCODONE | Partial Agonist w/ acetaminophen hycodan = infant |
PROPOXYPHENE | Partial Agonist |
NALOXONE | Antagonist short duration |
NALTREXONE | Antagonist long duration preferred treat alcoholism |
TRAMADOL | Opioid and antidepressant cross increase NE 5HT, weak mu |
Metabolism of Opioid | Hepatic viz conjugation with glucoronic acid mostly in kidney and some in bile most do not cross blood brain barrier |
Adverse effects of Opioid | miosis respiratory and cardiac depression sedation nausea and vomiting constipation postural hypotension tolerance and physical dependence |
What is the mechanism of Tolerance? | G-protein system- ligand binds at C-terminus -> recruit B arrestins - in clathrin coated pit ->inactivate more pits with more drugs |